The palladium‐mediated N ‐arylation of indoles with 4‐[ 18 F]fluoroiodobenzene as a novel radiolabelling method has been developed. Optimized reaction conditions were elaborated by variation of different catalyst systems (CuI/1,2‐diamines and Pd 2 (dba) 3 /phosphine ligands), bases and solvents in the reaction of indole with 4‐[ 18 F]fluoroiodobenzene. Optimized reaction conditions (Pd 2 (dba) 3 /(2‐(dicyclohexyl‐phosphino)‐2′‐( N , N ‐dimethylamino)‐biphenyl, NaOBu t , toluene, 100°C for 20 min) were applied for the synthesis of 18 F‐labelled σ 2 receptor ligands [ 18 F]‐11 and [ 18 F]‐13 which were obtained in 91 and 84% radiochemical yields, respectively.
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Wüst et al. (2004) studied this question.